公开(公告)号：WO9965870A3

公开(公告)日：2001-03-15

申请号：PCT/US9913744

申请日：1999-06-17

Applicant: VERTEX PHARMA ,  SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561 ,  A61K31/27 ,  A61K31/34 ,  A61K31/395 ,  C07D215/48

CPC classification number: C07D213/30 ,  C07C311/48 ,  C07C311/49 ,  C07C2601/08 ,  C07C2601/14 ,  C07D215/48 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D309/22 ,  C07D319/06 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract translation: 本发明涉及一类新型的磺酰胺，它们是天冬氨酰蛋白酶抑制剂。 在一个实施方案中，本发明涉及以特定结构和物理化学特征为特征的新型HIV天冬氨酰蛋白酶抑制剂。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制HIV-1和HIV-2蛋白酶活性，因此可有利地用作针对HIV-1和HIV-2病毒的抗病毒剂。 本发明还涉及使用本发明化合物抑制HIV天冬氨酰蛋白酶的活性的方法和用于筛选抗HIV活性化合物的方法。

公开(公告)号：DK1086076T3

公开(公告)日：2005-03-29

申请号：DK99928769

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： HALE MICHAEL R ,  SHERRILL RONALD GEORGE ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE W III ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：BR9912169A

公开(公告)日：2001-04-10

申请号：BR9912169

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：NO20006405A

公开(公告)日：2001-02-19

申请号：NO20006405

申请日：2000-12-15

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS III CLARENCE WEBSTER ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561 ,  C07C

CPC classification number: C07D213/30 ,  C07C311/48 ,  C07C311/49 ,  C07C2601/08 ,  C07C2601/14 ,  C07D215/48 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D309/22 ,  C07D319/06 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

公开(公告)号：OA11573A

公开(公告)日：2004-07-01

申请号：OA1200000350

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： WEBSTER ANDREWS CLARENCE III ,  FURFINE ERIC STEVEN ,  HALE MICHAEL R ,  LOWEN GREGORY THOMAS ,  SHERRILL RONALD GEORGE ,  SPALTENSTEIN ANDREW

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：AU767728B2

公开(公告)日：2003-11-20

申请号：AU4576099

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：AU4576099A

公开(公告)日：2000-01-05

申请号：AU4576099

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：CA2335477C

公开(公告)日：2010-11-30

申请号：CA2335477

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS CLARENCE WEBSTER III ,  LOWEN GREGORY THOMAS

IPC: C07D493/04 ,  A61K31/34 ,  A61K31/351 ,  A61K31/36 ,  A61K31/4184 ,  A61K31/426 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/5395 ,  A61K31/551 ,  A61K31/635 ,  A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

公开(公告)号：AU2007234578A1

公开(公告)日：2007-12-13

申请号：AU2007234578

申请日：2007-11-21

Applicant: VERTEX PHARMA

Inventor： FURFINE ERIC ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  LOWEN GREGORY THOMAS ,  ILL CLARENCE WEBSTER ANDREWS ,  SHERRILL RONALD GEORGE

IPC: C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

公开(公告)号：AP1717A

公开(公告)日：2007-01-30

申请号：AP2000002023

申请日：1999-06-17

Applicant: VERTEX PHARMA

Inventor： SHERRILL RONALD GEORGE ,  HALE MICHAEL R ,  SPALTENSTEIN ANDREW ,  FURFINE ERIC STEVEN ,  ANDREWS III CLARENCE WEBSTER ,  LOWEN GREGORY THOMAS

IPC: A61P31/18 ,  C07C303/00 ,  C07C311/48 ,  C07C311/49 ,  C07D213/30 ,  C07D235/06 ,  C07D235/26 ,  C07D235/30 ,  C07D235/32 ,  C07D241/42 ,  C07D243/04 ,  C07D265/02 ,  C07D277/30 ,  C07D307/20 ,  C07D309/06 ,  C07D309/12 ,  C07D319/06 ,  C07D405/12 ,  C07D407/12 ,  C07D413/06 ,  C07D417/12 ,  C07D493/04 ,  C07F9/6561

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.